The resolution of 1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-benzodiazepin-4-one (6)-(R,S)-2 was accomplished by chiral HPLC. The absolute configuration of (þ)-2, determined by X-ray crystallographic analysis, was R. The in vivo anticonvulsant activity of the enantiomers (þ)-(R)-2 and ()-(S)-2 is reported. It has been also demonstrated that compound (6)-(R,S)-2 in vivo undergoes oxidative metabolism to derivative 1.
Enantioseparation, absolute configuration determination, and anticonvulsant activity of (+/-)-1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro)-4H-2,3-be nzodiazepin-4-one
CALABRO', Maria;FICARRA, Paola;BRUNO, Giuseppe;ZAPPALA', Maria;MICALE, Nicola;GRASSO, Silvana
2007-01-01
Abstract
The resolution of 1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-benzodiazepin-4-one (6)-(R,S)-2 was accomplished by chiral HPLC. The absolute configuration of (þ)-2, determined by X-ray crystallographic analysis, was R. The in vivo anticonvulsant activity of the enantiomers (þ)-(R)-2 and ()-(S)-2 is reported. It has been also demonstrated that compound (6)-(R,S)-2 in vivo undergoes oxidative metabolism to derivative 1.File in questo prodotto:
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